Relationship of CYP2D6 genetic polymorphisms and the pharmacokinetics of tramadol in Chinese volunteers |
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| Authors: | Q. Li PhD R. Wang MD Y. Guo PhD S. Wen PhD L. Xu MD S. Wang PhD |
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| Affiliation: | 1. Department of Pharmacology, Tianjin Medical University, Tianjin;2. Department of Clinical Pharmacology, Chinese People Liberation Army General Hospital, Beijing;3. Beijing Institute of Radiation Medicine, Academy of Military Medical Sciences, Beijing, China |
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| Abstract: | Objective: To investigate the relationship between CYP2D6 genetic polymorphisms and the pharmacokinetics of tramadol in Chinese volunteers. Method: A gene chip was established for determining CYP2D6 genotype. Forty adult healthy Chinese subjects were categorized as: group 1, CYP2D6*1/*1; group 2, CYP2D6*2/*2; group 3, CYP2D6*2/*10; group 4, CYP2D6*10/*10. After oral administration of 100 mg tramadol, plasma and urine samples were collected over a 32‐h period. Results: The main pharmacokinetic parameters of tramadol and its metabolite O‐demethyltramadol (M1) in groups 1 and 2 were not significantly different. However, they were significantly different between groups 3 and 1, groups 4 and 1 and groups 4 and 3. Conclusion: CYP2D6*2 does not alter the pharmacokinetics of tramadol, whereas CYP2D6*10 did with homozygotes showing a more pronounced reduction than heterozygotes. The 32‐h metabolic ratio of tramadol to M1 were (mean ± SD) 2·05 ± 1·01, 2·13 ± 0·83, 4·24 ± 2·75 and 6·85 ± 2·78, respectively, in CYP2D6*1/*1, CYP2D6*2/*2, CYP2D6*2/*10 and CYP2D6*10/*10 subjects, respectively. |
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| Keywords: | CYP2D6 DNA microarray genetic polymorphisms pharmacogenomics tramadol |
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